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Tocris/GSK 429286/3726/10/10 mg

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货号: 3726/10

品牌: Tocris

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Description: Selective Rho-kinase (ROCK) inhibitor

Alternative Names: GSK429286A

Chemical Name: 4-[4-(Trifluoromethyl)phenyl]-N-(6-Fluoro-1H-indazol-5-yl)-2-methyl-6-oxo-1,4,5,6-tetrahydro-3-pyridinecarboxamide

Purity: ≥97% (HPLC)

Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity

Selective Rho-kinase inhibitor (IC₅₀ values are 14, 780 and 1940 nM for ROCK1, RSK and p70S6K respectively). Reverses adrenalin-induced contraction of the rat aortic ring (IC₅₀ = 190 nM) and causes a dose-dependent decrease in mean arterial blood pressure in spontaneous hypertensive rats. Orally active.

Licensing Information

Sold for research purposes under agreement from GlaxoSmithKline

Compound Libraries

GSK 429286 is also offered as part of the Tocriscreen Plus and Tocriscreen Stem Cell Toolbox. Find out more about compound libraries available from Tocris.

Technical Data

M. Wt	432.37
Formula	C₂₁H₁₆F₄N₄O₂
Storage	Store at +4°C
Purity	≥97% (HPLC)
CAS Number	864082-47-3
PubChem ID	11373846
InChI Key	OLIIUAHHAZEXEX-UHFFFAOYSA-N
Smiles	O=C1CC(C2=CC=C(C(F)(F)F)C=C2)C(C(NC3=C(F)C=C(NN=C4)C4=C3)=O)=C(C)N1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

All Tocris products are intended for laboratory research use only.

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	43.24	100
	ethanol	10.81	25

Preparing Stock Solutions

The following data is based on the product molecular weight 432.37. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	2.31 mL	11.56 mL	23.13 mL
5 mM	0.46 mL	2.31 mL	4.63 mL
10 mM	0.23 mL	1.16 mL	2.31 mL
50 mM	0.05 mL	0.23 mL	0.46 mL

Product Datasheets

Certificate of Analysis / Product Datasheet

Safety Datasheet

References

References are publications that support the products' biological activity.

Goodman et al (2007) Development of dihydropyridone indazole amides as selective rho-kinase inhibitors. J.Med.Chem. 50 6 PMID: 17201405

Nichols et al (2009) Substrate specificity and inhibitors of LRRK2, a protein kinase mutated in Parkinson's disease. Biochem.J. 424 47 PMID: 19740074

Keywords: GSK 429286, supplier, Selective, Rho-kinases, ROCK, inhibitors, inhibits, Rho-Associated, Coiled-Coil, Kinases, p160ROCK, ROK, GSK429286, GlaxoSmithKline, GSK, GSK429286A, GSK429286A, Rho-kinases, Rho-kinases, Tocris Bioscience

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